Methadone
was invented in 1937 by German scientists
Max Bockmühl and Gustav
Ehrhart at IG
Farben, who dubbed the chemical Hoechst 10820, and later named it Polamidon.[1] The
drug was not mass-produced for commercial use at all during World War II,
but after the war, the factory that produced the drug fell under American
control which spawned the start of the first clinical trials for methadone.
Many believe the myth that the brand, Dolophine, was coined in honor of
Adolf Hitler; however, the name was created by Eli-Lilly, an American pharmaceutical
company, perhaps a combination of the Latin word dolor (pain)
and the French word fin (end).
The word dol is also used in pain research to measure the level
of pain, e.g. 1 dol = 1 unit of pain.[2]
After Eli-Lilly introduced methadone as an analgesic, doctors thought it would be the next great painkiller, but by the early 1950s, it was barely being used. Then, in 1964, Dr. Marie Nyswander and Dr. Vincent Dole of Rockefeller University in New York began to research possible treatments for heroin addiction, and after reading about methadone in medical literature they began a clinical trial. Their clinical trials eventually developed into the first study of opioid substitution therapy. This resulted in a huge breakthrough in the field of addiction studies. Until this point, drug addiction was viewed as a character flaw, and this showed addiction is a treatable disease. Methadone maintenance therapy has been the most successful pharmacotherapy treatment of drug addiction in history.[3]
Chemical Names. 6-dimethylamino-4,4-diphenyl-3-heptan-one.
Classification. Opioid.
Primary Uses. Analgesia,
Opioid dependency treatment.
Other Names. Dolophine,
Methadose.
Pharmacology and Pharmacokinetics
Methadone is a synthetic narcotic analgesic, and full opioid agonist with multiple actions similar to those of morphine, which mostly affect the central nervous system and organs composed of smooth muscle.[4] Methadone is metabolized very slowly, and has a half-life ranging from 15-60 hours. The long half-life allows for once-a-day dosing for the treatment of opioid dependency. When taken to control pain, it must be taken 2-3 times per day because the analgesic activity lasts significantly shorter, than its pharmacological half-life. Methadone also has the unique property of having an affinity for NMDA (N-methyl-D-aspartic acid) receptors. NMDA is thought to regulate psychic dependence and tolerance via opioid antagonist-like activity.[5]
In
the United States, methadone is a Schedule II substance, making it illegal
to use/possess without a prescription. Schedule II substances, such as
dextroamphetamine, oxycodone,
and cocaine, meet the following criteria according to the Controlled
Substances Act:
- The drug or other substance has a high potential for abuse.
- The drug or other substance has a currently accepted medical use in treatment in the United States (or) a currently accepted medical use with severe restrictions.
- Abuse of the drug may lead to severe psychological or physical dependence.
Pain relief
Euphoria/dysphoria
Disorientation
Lightheadedness
Dizziness
Mood changes
Anxiety/reduced anxiety
Sedation
Itching
Nausea/vomiting
Decreased libido (sex drive)
Constipation
Facial flushing
Vertigo
If methadone is tapered correctly, withdrawal symptoms will be minimal; however, if a person jumps off of methadone cold turkey, withdrawal can be awful. Some medical professionals claim that methadone withdrawal is not as intense as heroin or oxycodone withdrawal, but recovering addicts are finding out the hard way that methadone withdrawal can be just as intense, not to mention much longer. Methadone withdrawal will last at least one week, but usually lasts about 2-3 weeks. Patients have stated that many withdrawal symptoms can linger for months after complete cessation. Withdrawal symptoms may include:
- Insomnia
- Bone/muscle pain
- Restlessness
- Anxiety
- Increased blood pressure
- Gooseflesh
- Cold sweats
- Chills
- Diarrhea
Additional Information
[1] History of Methadone. Narconon Southern
California. 2001. Accessed: May 3, 2007. [link]
[2] Joycelyn Woods. How Methadone Works. National
Alliance of Methadone Advocates. Accessed: May 3, 2007. [link]
[3] Methadone - Wikipedia. Wikipedia.
2 May 2007. Accessed: May 3, 2007. [link]
[4] Dolophine (Methadone) Clinical
Pharmacology. RxList - The Internet
Drug Index. 2007. Accessed: May 3, 2007. [link]
[5] DrugBank: Methadone. DrugBank. Accession Number: APRD00485.
27 June 2005. Accessed: May 3, 2007. [link]